- Molecular NameImatinib
- SynonymImatinib Mesylate; Imatinib Methansulfonate
- Weight493.615
- Drugbank_IDDB00619
- ACS_NO152459-95-5
- Show 3D model
- LogP (experiment)3.218
- LogP (predicted, AB/LogP v2.0)3.63
- pkaN/A
- LogD (pH=7, predicted)2.96
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)-3.64
- LogSw (predicted, AB/LogsW2.0)0.1
- Sw (mg/ml) (predicted, ACD/Labs)0.03
- No.of HBond Donors2
- No.of HBond Acceptors8
- No.of Rotatable Bonds7
- TPSA86.28
- StatusFDA approved
- AdministrationN/A
- PharmacologyA drug used to treat certain types of cancer.
- Absorption_value98.0
- Absorption (description)Imatinib is rapidly absorbed when given by mouth, and is highly bioavailable: 98% of an oral dose reaches the bloodstream.
- Caco_2N/A
- Bioavailability98.0
- Protein binding95.0
- Volume of distribution (VD)6.2 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmMetabolism of imatinib occurs in the liver and is mediated by several isozymes of the cytochrome P450 system, including CYP3A4 and, to a lesser extent, CYP1A2, CYP2D6, CYP2C9, and CYP2C19. The main metabolite, N-demethylated piperazine derivative, is also active.
- Half life18 h (imatinib), 40 h (active metabolite)
- ExcretionThe major route of elimination is in the bile and feces; only a small portion of the drug is excreted in the urine. Most of imatinib is eliminated as metabolites, only 25% is eliminated unchanged. The half-lives of imatinib and its main metabolite are 18 and 40 hours, respectively.
- Urinary Excretion5
- Clerance3.3 ml/min/kg
- ToxicitySide effects include nausea, vomiting, diarrhea, loss of appetite, dry skin, hair loss, swelling (especially in the legs or around the eyes) and muscle cramps
- LD50 (rat)N/A
- LD50 (mouse)N/A